Enantioselective, Catalytic Vicinal Difluorination of Alkenes
作者:Felix Scheidt、Michael Schäfer、Jérôme C. Sarie、Constantin G. Daniliuc、John J. Molloy、Ryan Gilmour
DOI:10.1002/anie.201810328
日期:2018.12.10
The enantioselective, catalytic vicinal difluorination of alkenes is reported by II/IIII catalysis using a novel, C2‐symmetric resorcinol derivative. Catalyst turnover via in situ generation of an ArIIIIF2 species is enabled by Selectfluor oxidation and addition of an inexpensive HF–amine complex. The HF:amine ratio employed in this process provides a handle for regioselective orthogonality as a function
I / I III催化使用新型C 2对称间苯二酚衍生物进行烯烃的对映选择性催化邻位二氟化反应。通过Selectfluor氧化和添加廉价的HF-胺络合物,可以原位生成ArI III F 2物种进行催化剂转换。此过程中使用的HF:胺比率为布朗选择性酸度的区域选择性正交性提供了一个解决方案。公开了从1,1-二氟化途径(基因)向所需的1,2-二氟化途径(邻位)的选择性逆转(两个方向均> 20:1)。用电子不足的苯乙烯进行验证有助于产生古老的CF 3的手性生物等排体药物发现中普遍使用的单元(20个示例,最高94:06 er)。还使用p- TolI(高达> 95%的收率)显示了反应的非手性变体。
Isoquinolinone compounds are provided that are useful for the inhibition of ADP-platelet aggregation, particularly in the treatment of thrombosis and thrombosis related conditions or disorders.
The invention provides novel imidazo-pyrazine derivatives having the general formula (I), and pharmaceutically acceptable salts thereof, wherein X, m, n, and R1 to R3 are as described herein: formula (I). Further provided are pharmaceutical compositions including the compounds, processes of manufacturing the compounds and methods of using the compounds as medicaments, in particular methods of using the compounds as antibiotics for the treatment or prevention of bacterial infections and resulting diseases.
Thermal Switchability of N-Chelating Hoveyda-type Catalyst Containing a Secondary Amine Ligand
作者:Karolina Żukowska、Anna Szadkowska、Aleksandra E. Pazio、Krzysztof Woźniak、Karol Grela
DOI:10.1021/om2011062
日期:2012.1.9
An investigation of aza analogues of the popular Hoveyda–Grubbs catalystcontaining a secondaryamineligand is presented, proving the crucial impact of steric as well as electronic factors on the catalyst’s stability and performance. The issue of latency in the reactivity profile of studied catalysts is examined, followed by structural and application studies.
[EN] PROTEIN INHIBITOR OR DEGRADING AGENT, PHARMACEUTICAL COMPOSITION CONTAINING SAME AND PHARMACEUTICAL USE<br/>[FR] INHIBITEUR DE PROTÉINE OU AGENT DE DÉGRADATION, COMPOSITION PHARMACEUTIQUE LE CONTENANT ET UTILISATION PHARMACEUTIQUE<br/>[ZH] 蛋白抑制剂或降解剂、包含其的药物组合物及医药上的用途